Synthesis and biological evaluation of C-13, C-14 modified taxane analogues from 1-deoxybaccatin VI

Abstract

Four C-13, C-14 side chain modified 9(R)-hydroxy-1-deoxy-taxane analogues 15, 16, 19 and 22 were semi-synthesized from 1-deoxybaccatin VI. The in vitro antitumor activity of these compounds was evaluated against A549 and A2780 cell lines. The preliminary SAR analysis showed that introduction of oxygen-containing group on C-14 could improve the cytotoxic activities.

Keywords:

• 1-Deoxybaccatin VI
• Taxane
• Cytotoxicity
• Oxidation
• Synthesis

Acknowledgments

The authors thank Drs. H. Deng and M. Shao, The Instrumental Analysis& Research Center of Shanghai University, for structural analysis.